| Company Name: |
ChemeGen |
| Tel: |
18818260767 |
| Email: |
2625930290@qq.com |
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| | PDE4B Inhibitor Basic information |
| Product Name: | PDE4B Inhibitor | | Synonyms: | PDE4B Inhibitor;KVA-D-88;PDE4B Inhibitor,PDE-4B Inhibitor;Methanone, [1-(3,4-dichlorophenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl](3,3-difluoro-1-azetidinyl)-;1-(3,4-dichlorophenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl](3,3-difluoro-1-azetidinyl)-methanone | | CAS: | 2410550-31-9 | | MF: | C17H11Cl2F2N3O | | MW: | 382.19 | | EINECS: | | | Product Categories: | | | Mol File: | 2410550-31-9.mol |  |
| | PDE4B Inhibitor Chemical Properties |
| Boiling point | 464.1±45.0 °C(Predicted) | | density | 1.55±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml | | form | A crystalline solid | | pka | 2.98±0.30(Predicted) |
| | PDE4B Inhibitor Usage And Synthesis |
| Biological Activity | PDE4B inhibitor is an inhibitor of phosphodiesterase 4B (PDE4B; IC50 = 140 nM).1,2 It is selective for PDE4B over a panel of 20 PDE isoforms and a panel of 39 CNS receptors at 10 μM but does inhibit the activity of PDE4C1, PDE3B, the serotonin (5-HT) receptor subtype 5-HT2C, and sigma-2 (σ2) receptors by greater than 50%.1 PDE4B inhibitor (1 μM) decreases LPS- or Pam3Cys-induced production of TNF-α in mouse bone marrow-derived macrophages (BMDMs). It reduces cocaine self-administration and the progressive ratio breakpoint in mice when administered at a dose of 5 mg/kg.2 | | References | 1.Vadukoot, A.K., Sharma, S., Aretz, C.D., et al.Synthesis and SAR studies of 1H-pyrrolo[2,3-b]pyridine-2-carboxamides as phosphodiesterase 4B (PDE4B) inhibitorsACS Med. Chem. Lett.11(10)1848-1854(2020)
2.Burkovetskaya, M.E., Liu, Q., Vadukoot, A.K., et al.KVA-D-88, a novel preferable phosphodiesterase 4B inhibitor, decreases cocaine-mediated reward properties in vivoACS Chem. Neurosci.11(15)2231-2242(2020) |
| | PDE4B Inhibitor Preparation Products And Raw materials |
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